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Sitagliptin Phosphate USP + Metformin Hydrochloride BP

Taglimet 50/500 tablet 50 mg + 500 mg 30's Tablet
Taglimet 50/1000 tablet 50 mg +1000 mg 30's Tablet


Taglimet 50/500 Tablet: Each film coated tablet contains Sitagliptin Phosphate (Monohydrate) USP 64.25 mg eq. to Sitagliptin 50 mg & Metformin HCl BP 500 mg. Taglimet 50/1000 Tablet:Each film coated tablet contains Sitagliptin Phosphate (Monohydrate) USP 64.25 mg eq. to Sitagliptin 50 mg & Metformin HCl BP 1000 mg.

Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, and Metformin hydrochloride (HCl), a biguanide, indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Sitagliptin The DPP-4 inhibitors are a class of agents that act as incretin enhancers. By inhibiting the DPP-4 enzyme, sitagliptin increases the levels of two known active incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. Sitagliptin is a potent and highly selective inhibitor of the enzyme DPP-4 and does not inhibit the closely-related enzymes DPP-8 or DPP-9 at therapeutic concentrations. Metformin HCl Metformin improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. With metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin response may actually decrease.

Combination of Sitagliptin and Metformin indicated as an adjunct to diet and exercise to improve glycaemic control in patients inadequately controlled on their maximal tolerated dose of metformin alone or those already being treated with the combination of sitagliptin and metformin. Combination of Sitagliptin and Metformin is indicated in combination with a sulphonylurea (i.e., triple combination therapy) as an adjunct to diet and exercise in patients inadequately controlled on their maximal tolerated dose of metformin and a sulphonylurea. Combination of Sitagliptin and Metformin is also indicated as add-on to insulin (i.e., triple combination therapy) as an adjunct to diet and exercise to improve glycaemic control in patients when stable dose of insulin and metformin alone do not provide adequate glycaemic control.

The dosage of Taglimet should be individualized on the basis of the patient's current regimen, effectiveness and tolerability while not exceed­ ing the maximum recommended dailydose of 100 mgsitagliptin and 2000 mg metformin. Initial combination therapy or maintenance of combination therapy should be individualized and left to the discretion of the health care provider. Taglimet should generally be given twice daily with meals, with gradual dose escalation, to reduce the gastrointestinal {GI) side effects due to metformin. The starting dose of Taglimet should be based on the patient's current regimen. The recommended starting dose in patients not currently treated with metformin is 50 mg sitagliptin/500 mg metformin hydrochloride twice daily, with gradual dose escalation recom­ mended to reduce gastrointestinal side effects associated with metformin. The starting dose in patients already treated with metformin should provide sitagliptin dosed as 50 mg twice daily {100 mg total daily dose) and the dose of metformin already being taken. For patients taking metformin 850 mg twicedaily, the recommended startingdose ofTaglimet is 50 mg sitagliptin/1000 mg metformin hydrochloride twice daily. Co-ad­ ministration of Taglimet with an insulin secretagogue {e.g.,sulfonylurea) or insulin may require lower doses of the insulin secretagogue or insulin to reduce the risk of hypoglycemia. No studies have been performed specifically examining the safety and efficacy of Glipite-M in patients previously treated with other oral antihypergtycemic agents and switched to Taglimet. Any change in therapy of type 2 diabetes should be undertak­ en with care and appropriate monitoring as changes in grycemic control can occur.

The most common adverse reactions reported in >5% of patients simulta­neously started on sitagliptin and metformin and more commonly than in patients treated with placebo were diarrhea, upper respiratory tract infection and headache. Nasopharyngitis was the only adverse reaction reported in 5% of patients treated with sitagliptin monotherapy. Hypogly­cemia was also reported more commonly in patients treated with the combination of Sitagliptin and sulfonylurea, with or without Metformin, than in patients given the combination of placebo and sulfonylurea, with or without Metformin. The most common established adverse reactions due to initiation of metformin therapy are diarrhea, nausea/vomiting, flatulence, abdominal discomfort, indigestion, asthenia, and headache.

Lactic acidosis is a rare but serious, metabolic complication that can occur due to metformin accumulation during treatment with Sitaglipfini Metformin HCI combination; when it occurs, it is fatal in approximately 50% of cases. Lactic acidosis may also occur in association with a number of pathophysiologic conditions, including diabetes mellitus and whenever there is significant tissue hypoperfusion and hypoxemia. There have been postmarketing reports of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis, in patients taking Sitagliptin/Metformin HCI combination. After initiation of Sitagliptin/Met­formin HCI combination, patients should be observed carefully for signs and symptoms of pancreatitis, If pancreatitis is suspected, Sitagliptin/Met­formin HCI combination should promptly be discontinued and appropriate management should be initiated. It is unknown whether patients with a history of pancreatitis are at increased risk for the development of pancre­atitis while using Sitagliptin/Metformin HCI combination. Since impaired hepatic function has been associated with some cases of lactic acidosis, Sitagliptin/Metformin HCI combination should generally be avoided in patients with clinical or laboratory evidence of hepatic disease. Metformin and sitagliptin are known to be substantially excreted by the kidney. The risk of metformin accumulation and lactic acidosis increases with the degree of impairment of renal function. Thus, patients with serum creatinine levels above the upper limit of normal for their age should not receive Sitagliptin/Metformin HCI combination. In the elderly, Sitaglipt­in/Metformin HCI combination should be carefully titrated to establish the minimum dose for adequate glycemic effect, because aging can be associated with reduced renal function.

Use in Pregnancy and Lactation Pregnancy: Pregnancy category B. There are no adequa1e and vvellcontrolled studies in pregnant women with Silagliptin/Metformin HCI combination or its individual components; therefore, the safety of Sitagliptin/Metformin HCI combination in pregnant women is not known. Sitagliptin/Metformin HCI combination should be used during pregnancy only if clearly needed. Sitagliptin: Reproduction studies have been performed in rats and rabbits. Doses of sitagliptin up to 125 mg/kg (approximately 12 times the human exposure at the maximum recommended human dose) did not impair fertility or harm the fetus. There are, however, no adequate and well controlled studies with sitagliptin in pregnant women. Metforrnin Hydrochloride: Metformin was not teratogenic in rats and rabbits at doses up to 600 mg/kg/day. This represents an exposure of about 2 and 6 times the maximum recommended human daily dose of 2,000 mg based on body surface area comparisons for rats and rabbits, respectively. Determination offetal concentrations demonstrated a partial placental barrier to metformin. Nursing Mothers: No studies in lactating animals have been conducted with the combined components of Sitagliptin/Metformin HCI combination. In studies performed with the individual components, both sitagliptin and metformin are secreted in the milk of lactating rats. It is not known whether sitagliptin is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Sitagliptin/Metformin HCI combination is administered to a nursing woman.

Cationic drugs {e.g., amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim or vancomycin) that are eliminated by renal tubular secretion theoretically have the potential for interaction with metformin by competing for common renal tubular transport systems. Such interaction between metformin and oral cimetidine has been observed in normal healthy volunteers in both single and multiple-dose metformin-cimetidine drug interaction studies, with a 60% increase in peak metformin plasma and whole blood concentrations and a 40% increase in plasma and whole blood metformin AUC. There was no change in elimination half-life in the single-dose study. There was a slight increase in the area under the curve (AUC, 11 %) and mean peak drug concentration {Cmax, 18%) of digoxin with the co-administration of 100 mg sitagliptin for 1 O day. These increases are not considered likely to be clinically meaningful. Digoxin, as a cationic drug, has the potential to compete with metformin for common renal tubular transport systems, thus affecting the serum concentrations of either digoxin, metformin or both. Patients receiving digoxin should be monitored appropriately. No dosage adjustment of digoxin or Glipitae-M is recommended. Certain drugs tend to produce hyperglycemia and may lead to loss of glycemic control. These drugs include the thiazides and other diuretics, corticoste­roids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs and isoniazid. When such drugs are administered to a patient receiving Sitagliptin/Metformin HCI combination the patient should be closely observed to maintain adequate glycemic control.

Overdose In the event of an overdose, it is reasonable to employ the usual support­ive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring {including obtaining an electrocardio­gram) and institute supportive therapy as indicated by the patient's clinical status. Sitagliptin is modestly dialyzable. In clinical studies, approximately 13.5% of the dose was removed over a 3- to 4-hour hemodialysis session. Prolonged hemodialysis may be considered if clinically appropriate. It is not known if sitagliptin is dialyzable by peritone­al dialysis. Metformin hydrochloride overdose of metformin hydrochloride has occurred, including ingestion of amounts greater than 50 grams. Hypoglycemia was reported in approximately 10% of cases, but no causal association with metformin hydrochloride has been established. Lactic acidosis has been reported in approximately 32% of metformin overdose cases. Metformin is dialyzable with a clearance of up to 170 mUmin under good hemodynamic conditions. Therefore, hemodialysis may be useful for removal of accumulated drug from patients in whom metformin overdosage is suspected.

Store in a cool (below 30°C) and dry place. Keep out of the reach of the children.

Sitagliptin/Metformin HCI combination is contraindicated in patients with: Renal disease or renal dysfunction, e.g., as suggested by serull) creatinine levels 0.5 mg/dL [males], 21 .4 mg/dL (females] or abnormal> creatinine clearance which may also result from conditions such as cardiovasaJlar collapse {shock), acute myocardial infarction and septicemia; acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma; history of a serious hypersensitivity reaction to Sitaglipt­in/Metformin HCI combination or Sitagliptin such as anaphylaxis or angioedema. This combination drugs should be temporarily discontinued in patients undergoing radiologic studies involving intravascular adminis­tration of iodinated contrast materials, because use of such products may result in acute alteration of renal function.

Taglimet 50/500: Each box contains 3 * 10 tablets in blister packs. Taglimet 50/1000: Each box contains 3 * 10 tablets in blister packs.